Optimized arylomycins are a new class of Gram-negative antibiotics
Smith, Peter A, Koehler, Michael F T, Girgis, Hany S, Yan, Donghong, Chen, Yongsheng, Chen, Yuan, Crawford, James J, Durk, Matthew R, Higuchi, Robert I, Kang, Jing, Murray, Jeremy, Paraselli, Prasuna, Park, Summer, Phung, Wilson, Quinn, John G, Roberts, Tucker C, Rougé, Lionel, Schwarz, Jacob B, Skippington, Elizabeth, Wai, John, Xu, Min, Yu, Zhiyong, Zhang, Hua, Tan, Man-Wah, Heise, Christopher E
Published in Nature (London) (01.09.2018)
Published in Nature (London) (01.09.2018)
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Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres
Cohen, Frederick, Koehler, Michael F.T., Bergeron, Philippe, Elliott, Linda O., Flygare, John A., Franklin, Matthew C., Gazzard, Lewis, Keteltas, Stephen F., Lau, Kevin, Ly, Cuong Q., Tsui, Vickie, Fairbrother, Wayne J.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Membrane Permeability in a Large Macrocyclic Peptide Driven by a Saddle-Shaped Conformation
Faris, Justin H., Adaligil, Emel, Popovych, Nataliya, Ono, Satoshi, Takahashi, Mifune, Nguyen, Huy, Plise, Emile, Taechalertpaisarn, Jaru, Lee, Hsiau-Wei, Koehler, Michael F. T., Cunningham, Christian N., Lokey, R. Scott
Published in Journal of the American Chemical Society (21.02.2024)
Published in Journal of the American Chemical Society (21.02.2024)
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Structural basis for dual-mode inhibition of the ABC transporter MsbA
Ho, Hoangdung, Miu, Anh, Alexander, Mary Kate, Garcia, Natalie K, Oh, Angela, Zilberleyb, Inna, Reichelt, Mike, Austin, Cary D, Tam, Christine, Shriver, Stephanie, Hu, Huiyong, Labadie, Sharada S, Liang, Jun, Wang, Lan, Wang, Jian, Lu, Yan, Purkey, Hans E, Quinn, John, Franke, Yvonne, Clark, Kevin, Beresini, Maureen H, Tan, Man-Wah, Sellers, Benjamin D, Maurer, Till, Koehler, Michael F T, Wecksler, Aaron T, Kiefer, James R, Verma, Vishal, Xu, Yiming, Nishiyama, Mireille, Payandeh, Jian, Koth, Christopher M
Published in Nature (London) (01.05.2018)
Published in Nature (London) (01.05.2018)
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Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA
Alexander, Mary Kate, Miu, Anh, Oh, Angela, Reichelt, Mike, Ho, Hoangdung, Chalouni, Cecile, Labadie, Sharada, Wang, Lan, Liang, Jun, Nickerson, Nicholas N, Hu, Huiyong, Yu, Lan, Du, Miaofen, Yan, Donghong, Park, Summer, Kim, Janice, Xu, Min, Sellers, Benjamin D, Purkey, Hans E, Skelton, Nicholas J, Koehler, Michael F T, Payandeh, Jian, Verma, Vishal, Xu, Yiming, Koth, Christopher M, Nishiyama, Mireille
Published in Antimicrobial agents and chemotherapy (01.11.2018)
Published in Antimicrobial agents and chemotherapy (01.11.2018)
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GDC-0449—A potent inhibitor of the hedgehog pathway
Robarge, Kirk D., Brunton, Shirley A., Castanedo, Georgette M., Cui, Yong, Dina, Michael S., Goldsmith, Richard, Gould, Stephen E., Guichert, Oivin, Gunzner, Janet L., Halladay, Jason, Jia, Wei, Khojasteh, Cyrus, Koehler, Michael F.T., Kotkow, Karen, La, Hank, LaLonde, Rebecca L., Lau, Kevin, Lee, Leslie, Marshall, Derek, Marsters, James C., Murray, Lesley J., Qian, Changgeng, Rubin, Lee L., Salphati, Laurent, Stanley, Mark S., Stibbard, John H.A., Sutherlin, Daniel P., Ubhayaker, Savita, Wang, Shumei, Wong, Susan, Xie, Minli
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
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Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells
Koehler, Michael F. T, Bergeron, Philippe, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin R, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen H
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Potent Killing of Pseudomonas aeruginosa by an Antibody-Antibiotic Conjugate
Kajihara, Kimberly K, Pantua, Homer, Hernandez-Barry, Hilda, Hazen, Meredith, Deshmukh, Kiran, Chiang, Nancy, Ohri, Rachana, Castellanos, Erick R, Martin, Lynn, Matsumoto, Marissa L, Payandeh, Jian, Storek, Kelly M, Schneider, Kellen, Smith, Peter A, Koehler, Michael F T, Tsai, Siao Ping, Vandlen, Richard, Loyet, Kelly M, Nakamura, Gerald, Pillow, Thomas, Seshasayee, Dhaya, Kapadia, Sharookh B, Hazenbos, Wouter L W
Published in mBio (29.06.2021)
Published in mBio (29.06.2021)
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Lipid Tales: Optimizing Arylomycin Membrane Anchors
Koehler, Michael F. T., Chen, Yi-Chen, Chen, Yongsheng, Chen, Yuan, Crawford, James J., Durk, Matthew R., Garland, Keira, Hanan, Emily J., Higuchi, Robert I., Hu, Huiyong, Ly, Cuong Q., Paraselli, Prasuna G., Roberts, Tucker C., Schwarz, Jacob B., Smith, Peter A., Yu, Zhiyong, Heise, Christopher E.
Published in ACS medicinal chemistry letters (09.11.2023)
Published in ACS medicinal chemistry letters (09.11.2023)
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Journal Article
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8
Bergeron, Philippe, Koehler, Michael F. T, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Ramaswamy, Sreemathy, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2
Zak, Mark, Hurley, Christopher A, Ward, Stuart I, Bergeron, Philippe, Barrett, Kathy, Balazs, Mercedesz, Blair, Wade S, Bull, Richard, Chakravarty, Paroma, Chang, Christine, Crackett, Peter, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ellwood, Charles, Gaines, Simon, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Gribling, Peter, Hamman, Chris, Harstad, Eric, Hewitt, Peter, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Labadie, Sharada, Lee, Wyne P, Liao, Jiangpeng, Liimatta, Marya, Mendonca, Rohan, Narukulla, Raman, Pulk, Rebecca, Reeve, Austin, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, van Abbema, Anne, Aliagas, Ignacio, Avitabile-Woo, Barbara, Xiao, Yisong, Yang, Jing, Kulagowski, Janusz J
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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Quinazoline Sulfonamides as Dual Binders of the Proteins B-Cell Lymphoma 2 and B-Cell Lymphoma Extra Long with Potent Proapoptotic Cell-Based Activity
Sleebs, Brad E, Czabotar, Peter E, Fairbrother, Wayne J, Fairlie, W. Douglas, Flygare, John A, Huang, David C. S, Kersten, Wilhelmus J. A, Koehler, Michael F. T, Lessene, Guillaume, Lowes, Kym, Parisot, John P, Smith, Brian J, Smith, Morey L, Souers, Andrew J, Street, Ian P, Yang, Hong, Baell, Jonathan B
Published in Journal of medicinal chemistry (24.03.2011)
Published in Journal of medicinal chemistry (24.03.2011)
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Journal Article
Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
Zak, Mark, Mendonca, Rohan, Balazs, Mercedesz, Barrett, Kathy, Bergeron, Philippe, Blair, Wade S, Chang, Christine, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Hamman, Chris, Hanan, Emily J, Harstad, Eric, Hewitt, Peter R, Hurley, Christopher A, Jin, Tian, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Kulagowski, Janusz J, Labadie, Sharada, Liao, Jiangpeng, Liimatta, Marya, Lin, Zhonghua, Lupardus, Patrick J, Maxey, Robert J, Murray, Jeremy M, Pulk, Rebecca, Rodriguez, Madeleine, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, Ultsch, Mark, van Abbema, Anne, Ward, Stuart I, Xiao, Ling, Xiao, Yisong
Published in Journal of medicinal chemistry (12.07.2012)
Published in Journal of medicinal chemistry (12.07.2012)
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An integrated suite of modeling tools that empower scientists in structure- and property-based drug design
Feng, Jianwen A., Aliagas, Ignacio, Bergeron, Philippe, Blaney, Jeff M., Bradley, Erin K., Koehler, Michael F. T., Lee, Man-Ling, Ortwine, Daniel F., Tsui, Vickie, Wu, Johnny, Gobbi, Alberto
Published in Journal of computer-aided molecular design (01.06.2015)
Published in Journal of computer-aided molecular design (01.06.2015)
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Journal Article
Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single Agent Antiproliferative Activity
Koehler, Michael F. T, Bergeron, Philippe, Blackwood, Elizabeth, Bowman, Krista K, Chen, Yung-Hsiang, Deshmukh, Gauri, Ding, Xiao, Epler, Jennifer, Lau, Kevin, Lee, Leslie, Liu, Lichuan, Ly, Cuong, Malek, Shiva, Nonomiya, Jim, Oeh, Jason, Ortwine, Daniel F, Sampath, Deepak, Sideris, Steve, Trinh, Lan, Truong, Tom, Wu, Jiansheng, Pei, Zhonghua, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (27.12.2012)
Published in Journal of medicinal chemistry (27.12.2012)
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Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR)
Estrada, Anthony A, Shore, Daniel G, Blackwood, Elizabeth, Chen, Yung-Hsiang, Deshmukh, Gauri, Ding, Xiao, DiPasquale, Antonio G, Epler, Jennifer A, Friedman, Lori S, Koehler, Michael F. T, Liu, Lichuan, Malek, Shiva, Nonomiya, Jim, Ortwine, Daniel F, Pei, Zhonghua, Sideris, Steve, St-Jean, Frederic, Trinh, Lan, Truong, Tom, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (11.04.2013)
Published in Journal of medicinal chemistry (11.04.2013)
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Journal Article
A Putative Bacterial ABC Transporter Circumvents the Essentiality of Signal Peptidase
Morisaki, J Hiroshi, Smith, Peter A, Date, Shailesh V, Kajihara, Kimberly K, Truong, Chau Linda, Modrusan, Zora, Yan, Donghong, Kang, Jing, Xu, Min, Shah, Ishita M, Mintzer, Robert, Kofoed, Eric M, Cheung, Tommy K, Arnott, David, Koehler, Michael F T, Heise, Christopher E, Brown, Eric J, Tan, Man-Wah, Hazenbos, Wouter L W
Published in mBio (06.09.2016)
Published in mBio (06.09.2016)
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Structure-Guided Rescaffolding of Selective Antagonists of BCL-X L
Koehler, Michael F. T., Bergeron, Philippe, Choo, Edna F., Lau, Kevin, Ndubaku, Chudi, Dudley, Danette, Gibbons, Paul, Sleebs, Brad E., Rye, Carl S., Nikolakopoulos, George, Bui, Chinh, Kulasegaram, Sanji, Kersten, Wilhelmus J. A., Smith, Brian J., Czabotar, Peter E., Colman, Peter M., Huang, David C. S., Baell, Jonathan B., Watson, Keith G., Hasvold, Lisa, Tao, Zhi-Fu, Wang, Le, Souers, Andrew J., Elmore, Steven W., Flygare, John A., Fairbrother, Wayne J., Lessene, Guillaume
Published in ACS medicinal chemistry letters (12.06.2014)
Published in ACS medicinal chemistry letters (12.06.2014)
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Journal Article
Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine
Cohen, Frederick, Bergeron, Philippe, Blackwood, Elizabeth, Bowman, Krista K, Chen, Huifen, DiPasquale, Antonio G, Epler, Jennifer A, Koehler, Michael F. T, Lau, Kevin, Lewis, Cristina, Liu, Lichuan, Ly, Cuong Q, Malek, Shiva, Nonomiya, Jim, Ortwine, Daniel F, Pei, Zhonghua, Robarge, Kirk D, Sideris, Steve, Trinh, Lan, Truong, Tom, Wu, Jiansheng, Zhao, Xianrui, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (12.05.2011)
Published in Journal of medicinal chemistry (12.05.2011)
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